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公开(公告)号：US08298513B2
公开(公告)日：2012-10-30
申请号：US12525599
申请日：2008-02-05
IPC分类号： A61K49/00
CPC分类号： C07K1/13 , A61K49/0039 , A61K49/0041 , A61K49/0047 , A61K49/0056 , A61K49/0058 , A61K51/081 , A61K51/083 , A61K51/085 , A61K51/088 , A61K51/10 , A61K51/1093 , C07C229/44 , C07C237/04 , C07D271/12 , C07D311/16 , C07D311/90 , C07D413/12 , C07D495/04 , C07F5/02 , C07F7/1804
摘要： A label with which labeling is easy when labeling a molecule, i.e., a label that has a high reaction rate upon labeling and that produces a high reaction yield, as well as a precursor for the production of the label are provided. This is achieved by a hexatriene-β-carbonyl compound represented by Formula (I), a hexatriene-β-carbonyl compound represented by Formula (II), a hexatriene-β-carbonyl compound represented by Formula (III) and a hexatriene-β-carbonyl compound represented by Formula (IV). (wherein R1, R2, R3, R4, R5, X1, X2 and Z are as defined in the specification)
摘要翻译： 提供了标记分子时标签易于标记的标签，即标记时具有高反应速率并产生高反应产率的标记，以及用于生产标签的前体。 由式（I）表示的己三烯 - 羰基化合物，由式（II）表示的己三烯 - 羰基化合物，由式（III）表示的己三烯 - 羰基化合物和式 由式（Ⅳ）表示的己三烯 - 羰基化合物。 （其中R1，R2，R3，R4，R5，X1，X2和Z如说明书中所定义）
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公开(公告)号：US20100008857A1
公开(公告)日：2010-01-14
申请号：US12525599
申请日：2008-02-05
IPC分类号： A61K49/00 , C07D257/02 , C07D271/12 , C07D311/82 , C07K16/00
CPC分类号： C07K1/13 , A61K49/0039 , A61K49/0041 , A61K49/0047 , A61K49/0056 , A61K49/0058 , A61K51/081 , A61K51/083 , A61K51/085 , A61K51/088 , A61K51/10 , A61K51/1093 , C07C229/44 , C07C237/04 , C07D271/12 , C07D311/16 , C07D311/90 , C07D413/12 , C07D495/04 , C07F5/02 , C07F7/1804
摘要： A label with which labeling is easy when labeling a molecule, i.e., a label that has a high reaction rate upon labeling and that produces a high reaction yield, as well as a precursor for the production of the label are provided. This is achieved by a hexatriene-β-carbonyl compound represented by Formula (I), a hexatriene-β-carbonyl compound represented by Formula (II), a hexatriene-β-carbonyl compound represented by Formula (III) and a hexatriene-β-carbonyl compound represented by Formula (IV). (wherein R1, R2, R3, R4, R5, X1, X2 and Z are as defined in the specification)
摘要翻译： 提供了标记分子时标签易于标记的标签，即标记时具有高反应速率并产生高反应产率的标记，以及用于生产标签的前体。 由式（I）表示的六亚乙基-β-羰基化合物，式（II）表示的六亚乙基-β-羰基化合物，式（III）表示的六亚乙基-β-羰基化合物和六 （IV）表示的羰基化合物。 （其中R1，R2，R3，R4，R5，X1，X2和Z如说明书中所定义）
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公开(公告)号：US20120177571A1
公开(公告)日：2012-07-12
申请号：US13387357
申请日：2010-07-28
CPC分类号： A61K51/088 , A61K51/083 , C07K14/655 , G01N33/56966 , G01N2333/655
摘要： A pancreatic endocrine cell indicating agent of the present invention includes a modified polypeptide in which a metal chelator binds only to an amino acid that is located at a site other than a somatostatin receptor-binding active site in a polypeptide selected from the group consisting of somatostatin and somatostatin analogs; and a radioactive metal nuclide held by the metal chelator. According to the present invention, it is therefore possible to provide a novel pancreatic endocrine cell indicating agent.
摘要翻译： 本发明的胰内分泌细胞指示剂包括修饰的多肽，其中金属螯合剂仅结合位于除生长抑素受体结合活性位点之外的位点的氨基酸，所述多肽选自生长抑素 和生长抑素类似物; 和由金属螯合剂保持的放射性金属核素。 根据本发明，可以提供一种新型的胰内分泌细胞指示剂。
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公开(公告)号：US20110237774A1
公开(公告)日：2011-09-29
申请号：US13123137
申请日：2009-10-09
申请人： Koki Hasegawa , Yasuyoshi Watanabe
发明人： Koki Hasegawa , Yasuyoshi Watanabe
CPC分类号： C07K1/13 , A61K49/0002 , A61K51/10 , C07K1/1072 , C07K14/605 , C07K14/645 , C07K14/655 , Y02P20/55
摘要： The invention provides a method for introducing 1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (DOTA) into a compound such as a peptide. The method comprises a first step for preparing a mixed liquid of DOTA having no protecting group and dimethylsulfoxide, and a second step for contacting the mixed liquid with the compound carried on a solid-phase carrier.
摘要翻译： 本发明提供了将1,4,7,10-四氮杂环十二烷-N，N'，N“，N” - 四乙酸（DOTA）引入化合物如肽中的方法。 该方法包括：制备没有保护基和二甲基亚砜的DOTA的混合液的第一步骤，以及使混合液与载持在固相载体上的化合物接触的第二步骤。
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5.发明申请公开(公告)号：US20120263645A1
公开(公告)日：2012-10-18
申请号：US13517296
申请日：2010-12-22
申请人： Yasuyoshi Watanabe , Koki Hasegawa
发明人： Yasuyoshi Watanabe , Koki Hasegawa
CPC分类号： G01N33/5088 , A61K51/083 , A61N2005/1021 , C07K7/06 , C07K14/57563 , C07K14/605 , C07K2319/00 , C07K2319/20 , C07K2319/21 , C07K2319/23 , C07K2319/33 , C07K2319/41 , C07K2319/43 , C07K2319/50 , G01N33/60 , G01N2500/00
摘要： The present invention provides a clinically usable radiolabeled compound that is precisely directable in vivo to a target tissue. The compound of the present invention has a first polypeptide or an analogue thereof, and a second polypeptide bonded to an N-terminus of the first polypeptide or the analogue thereof. In the compound, the first polypeptide is a polypeptide that specifically binds with a protein expressed in a target tissue, the second polypeptide has an amino acid region that has a high affinity for a radioactive metal nuclide, and the radioactive metal nuclide that has a high affinity for the amino acid region is held in the amino acid region.
摘要翻译： 本发明提供临床可用的放射性标记化合物，其在体内可精确地指向靶组织。 本发明的化合物具有第一多肽或其类似物，以及与第一多肽或其类似物的N末端键合的第二多肽。 在化合物中，第一多肽是与靶组织中表达的蛋白质特异性结合的多肽，第二多肽具有对放射性金属核素具有高亲和力的氨基酸区域，并且具有高的放射性金属核素 对氨基酸区域的亲和性保持在氨基酸区域。
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6.发明授权Methods for carbon isotope labeling synthesis by transition metal-promoted carbonylation via isocyanate using azides and carbon-isotope monoxide 失效通过使用叠氮化物和碳同位素一氧化碳通过异氰酸酯过渡金属促进羰基化的碳同位素标记合成方法公开(公告)号：US08741261B2
公开(公告)日：2014-06-03
申请号：US11086632
申请日：2005-03-22
申请人： Bengt Langstrom , Julien Barletta , Hisashi Doi , Masaaki Suzuki , Ryoji Noyori , Yasuyoshi Watanabe , Farhad Karimi
发明人： Bengt Langstrom , Julien Barletta , Hisashi Doi , Masaaki Suzuki , Ryoji Noyori , Yasuyoshi Watanabe , Farhad Karimi
IPC分类号： A61K51/00 , A61M36/14 , C07D345/00 , C07D205/00 , C07D213/46
CPC分类号： C07C333/04 , A61K51/04 , A61K51/0453 , A61K51/0455 , C07B59/00 , C07B2200/05 , C07C231/10 , C07C269/02 , C07C273/1827 , C07C333/08 , C07D205/08 , C07D207/263 , C07D207/267 , C07D213/64 , C07C233/07 , C07C271/28 , C07C275/28 , C07C275/64
摘要： Methods and reagents for transition metal-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon-isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
摘要翻译： 提供了使用碳同位素标记的一氧化碳通过异氰酸酯过渡金属促进羰基化的方法和试剂。 所得碳同位素标记的化合物可用作放射性药物，特别用于正电子发射断层扫描（PET）。 还提供了用于PET研究的相关工具包。
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公开(公告)号：US20120230914A1
公开(公告)日：2012-09-13
申请号：US13381078
申请日：2010-07-05
申请人： Yasuyoshi Watanabe , Hirotaka Onoe , Kayo Takahashi , Masaaki Suzuki , Hisashi Doi , Takamitsu Hosoya
发明人： Yasuyoshi Watanabe , Hirotaka Onoe , Kayo Takahashi , Masaaki Suzuki , Hisashi Doi , Takamitsu Hosoya
IPC分类号： A61K49/00 , A61K51/04 , C07F7/22 , C07D249/14 , C07F5/05
CPC分类号： C07D249/08 , A61K51/0453 , C07B2200/05
摘要： A labeling compound of the present invention includes a structure represented by formula (1) wherein X1 is 11CH3, CH218F, CF218F, 18F, 76Br or 124I, X2 is CN or NO2, and R is any one of groups represented by or a structure represented by formula (2) wherein X3 is CH3, CH2F, CF3, F, Br or I, and R is defined equally as in the formula (1). This allows realizing a labeling compound for PET, capable of quantifying aromatase with high accuracy.
摘要翻译： 本发明的标记化合物包括由式（1）表示的结构，其中X1为11CH3，CH218F，CF218F，18F，76Br或124I，X2为CN或NO2，R为由 通式（2）其中X 3是CH 3，CH 2 F，CF 3，F，Br或I，R与式（1）同样地定义。 这允许实现PET的标记化合物，能够以高精度定量芳香化酶。
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公开(公告)号：US5700833A
公开(公告)日：1997-12-23
申请号：US594152
申请日：1996-01-31
IPC分类号： C07C51/09 , C07C59/54 , C07C69/732 , C07C59/11
CPC分类号： C07C59/54
摘要： The present invention provides novel isocarbacyclin derivatives useful for search and study of prostacyclin receptor and as a therapeutic drug for central nervous system diseases, which derivatives are expressed by the following formula �I!: ##STR1## �where, R.sup.1 represents a hydrogen atom, an alkyl group, or cation of an appropriate amount, and R.sup.2 an alkylene group.!
摘要翻译： 本发明提供了可用于前列环素受体的研究和研究的新型异卡波环素衍生物，作为中枢神经系统疾病的治疗药物，该衍生物由下式[I]表示：其中，R1表示 氢原子，烷基或适当量的阳离子，R 2为亚烷基。
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9.发明申请18F-LABELED AZIDE COMPOUND, REAGENT FOR 18F-LABELING AND METHOD FOR 18F-LABELING OF ALKYNE COMPOUND USING SAME 失效18F标记的AZIDE化合物，18F标记试剂和使用其的18K标记的烷基化合物的方法公开(公告)号：US20120101266A1
公开(公告)日：2012-04-26
申请号：US13320421
申请日：2010-05-14
申请人： Yasuyoshi Watanabe , Masaaki Suzuki , Hisashi Doi , Takeshi Kuboyama , Satoshi Obika , Takeshi Imanichi
发明人： Yasuyoshi Watanabe , Masaaki Suzuki , Hisashi Doi , Takeshi Kuboyama , Satoshi Obika , Takeshi Imanichi
IPC分类号： C07H1/00 , C07D249/06 , C07D249/04
CPC分类号： A61K51/0453 , A61K51/0491 , C07B59/005 , C07B2200/05 , C07C247/16 , C07D249/06
摘要： [OBJECT]The present invention provides an 18F-labeled azide compound usable in the Huisgen reaction which enables 18F-labeling although only a small quantity of alkyne compound is available as a counterpart substrate, more specifically the 18F-labeled azide compound enabling the PET to be applied to peptides or oligonucleotides and enabling the 18F-labeling of any sites of oligonucleotide other than the 5′ end or 3′ end thereof, a reagent for 18F-labeling, and a method for 18F-labeling of an alkyne compound using the same.[SOLVING MEANS]An 18F-labeled azide compound according to the present invention is expressed by the following structural formula 1.[SELECTED DRAWING] None
摘要翻译： 本发明提供了可用于Huisgen反应的18F标记的叠氮化合物，其能够进行18F标记，尽管只有少量的炔化合物可用作对应的底物，更具体地说，18F-标记的叠氮化合物使PET能够 应用于肽或寡核苷酸，并且使得除了5'末端或3'末端以外的寡核苷酸的任何位点的18F标记，用于18F标记的试剂和使用其的18E-标记的炔化合物的方法 。 [解决方案]根据本发明的18F标记的叠氮化合物由以下结构式1表示。[选择的图]无
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10.发明申请Methods for carbon istope labeling synthesis by rhodium-promoted carbonylation via isocyanate using azides and carbon-isotope monoxide 审中-公开通过使用叠氮化物和碳 - 同位素一氧化物的铑促进的通过异氰酸酯的羰基化的碳同位素标记合成方法公开(公告)号：US20070249816A1
公开(公告)日：2007-10-25
申请号：US10582761
申请日：2004-12-13
申请人： Bengt Langstrom , Julien Barletta , Hisashi Doi , Masaaki Suzuki , Ryoji Noyori , Yasuyoshi Watanabe , Farhad Karimi
发明人： Bengt Langstrom , Julien Barletta , Hisashi Doi , Masaaki Suzuki , Ryoji Noyori , Yasuyoshi Watanabe , Farhad Karimi
IPC分类号： C07D213/84 , C07C233/02 , C07D205/04
CPC分类号： A61K51/04 , C07B59/00 , C07B2200/05 , C07C263/00 , C07C269/02 , C07C273/1827 , C07C265/12 , C07C271/28 , C07C275/28
摘要： Methods and reagents for rhodium-promoted carbonylation via isocyanate using carbon-isotope labeled carbon monoxide are provided. The resultant carbon isotope labeled compounds are useful as radiopharmaceuticals, especially for use in Positron Emission Tomography (PET). Associated kits for PET studies are also provided.
摘要翻译： 提供了使用碳同位素标记的一氧化碳通过异氰酸酯进行铑促进羰基化的方法和试剂。 所得碳同位素标记的化合物可用作放射性药物，特别用于正电子发射断层扫描（PET）。 还提供了用于PET研究的相关工具包。
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